6-(10-羟基癸基)-2,3-二甲氧基-5-甲基-1,4-苯醌（艾地苯醌）及相关苯醌对猪胰腺磷脂酶A2活性的影响。

Effects of 6-(10-hydroxydecyl)-2,3-dimethoxy-5-methyl-1,4-benzoquinone (idebenone) and related benzoquinones on porcine pancreas phospholipase A2 activity.

作者信息

Amano T, Terao S, Imada I

机构信息

Research and Development Division, Takeda Chemical Ind. Ltd., Osaka, Japan.

出版信息

Biol Pharm Bull. 1995 May;18(5):779-81. doi: 10.1248/bpb.18.779.

DOI:10.1248/bpb.18.779

PMID:7493000

Abstract

6-(10-Hydroxydecyl)-2,3-dimethoxy-5-methyl-1,4-benzoquinone (idebenone) has been found to have a membrane-stabilizing activity in studies using lysosomes. Using dimyristoyl L-alpha-phosphatidylcholine (DMPC) as a substrate, the effects of idebenone and related benzoquinones on phospholipid digestion by phospholipase A2 (PLA2) was investigated. Free myristic acid, released from DMPC upon PLA2 treatment, was anthrylmethylated with 9-anthryldiazomethane (ADAM) and determined by reversed-phase HPLC. Idebenone and a related benzoquinone, 2,3-dimethoxy-5-methyl-6-(10-morpholinodecyl)-1, 4-benzquinone hydrochloride (QS-10.Mor), inhibited the hydrolysis of the substrate with PLA2 in a dose-dependent manner. It is suggested that the effect of idebenone on PLA2, in addition to its antioxidant activity lipid peroxidation, can be attributed to membrane-stabilizing activity.

摘要

在使用溶酶体的研究中发现，6-(10-羟基癸基)-2,3-二甲氧基-5-甲基-1,4-苯醌（艾地苯醌）具有膜稳定活性。以二肉豆蔻酰基-L-α-磷脂酰胆碱（DMPC）为底物，研究了艾地苯醌及相关苯醌对磷脂酶A2（PLA2）消化磷脂的影响。经PLA2处理后从DMPC释放的游离肉豆蔻酸，用9-蒽重氮甲烷（ADAM）进行蒽甲基化，并通过反相高效液相色谱法测定。艾地苯醌和一种相关苯醌，2,3-二甲氧基-5-甲基-6-(10-吗啉代癸基)-1,4-苯醌盐酸盐（QS-10.Mor），以剂量依赖方式抑制PLA2对底物的水解。提示艾地苯醌除其抗氧化活性（脂质过氧化）外，对PLA2的作用可归因于膜稳定活性。